Phosphinic acids derivatives, beta-secretase inhibitors for...

C - Chemistry – Metallurgy – 07 – F

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C07F 9/30 (2006.01)

Patent

CA 2544203

The present invention relates to phosphinic acid derivatives of formula (I) wherein R1 is aryl or heteroaryl, R2 is (C1-C5)-alkyl or phenyl, R3 is hydrogen, (C1-C5)-alky, O-(C1-C5)-alkyl or phenyl, R4 is (C1-C6)-alkyl, (C3- C6)-cycloalkyl, phenyl, pyridyl or indolyl, and pharmaceutically acceptable salts thereof. The compounds can be used in the treatment or prevention of a disease related to the inhibition of beta-secretase, inter alia for the treatment of Alzheimer~s disease.

La présente invention concerne des dérivés d'acide phosphinique de formule (I), dans laquelle R?1¿ représente un aryle ou un hétéroaryle, R?2¿ représente (C¿1?-C¿5?)-alkyle ou phényle, R?3¿ représente l'hydrogène, (C¿1?-C¿5?)-alkyle, O-(C¿1?-C¿5?)-alkyle ou phényle, R?4¿ représente (C¿1?-C¿6?)-alkyle, (C¿3?-C¿6?)-cycloalkyle, phényle, pyridyle ou indolyle, et des sels associés acceptables pharmaceutiquement. Ces composés peuvent être utilisés dans le traitement ou la prévention d'une maladie liée à l'inhibition de la bêta-sécrétase, notamment, dans le traitement de la maladie d'Alzheimer.

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